Structure- activity relationship study of nafuredin-gamma derivatives as complex I selective inhibitors
| Project/Area Number |
23590132
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Kitasato University |
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Principal Investigator |
ARIMA Shiho 北里大学, 薬学部, 助教 (20276158)
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| Project Period (FY) |
2011 – 2013
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2013: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2012: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2011: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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| Keywords | 医薬品化学 / 構造活性相関 |
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| Research Abstract |
Nafuredin-gamma, converted from nafuredin as a fungal metabolite under mild basic conditions, demonstrates inhibitory activity and selectivity against complex I of Ascaris suum. These compounds have unique and useful biological activities; however, the conjugated diene moieties included in the structure are highly unstable in the presence of oxygen. To solved this problem, stable nafuredin-gamma derivatives with non-conjugated (E)-olefins in the side chain moiety designed and synthesized. These derivatives showed moderate complex I inhibitory activities and high stabilities in air .
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Report
(4 results)
Research Products
(20 results)
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[Journal Article] Total synthesis and absolute configuration of avenolide, extracellular factor in Streptomyces avermitilis2011
Author(s)
Nagamitsu, T., Uchida, M., Takamatsu, S., Arima, S.Miyamoto, K., Kitani, S.Nihira, T., Ikeda, H.
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Journal Title
J Antibiotics Nature
Volume: 64
Issue: 12
Pages: 781-787
DOI
NAID
Related Report
Peer Reviewed
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